Project introduction:
Established in 2010, the target company focuses on small molecule medicines which are used for cancer and immune system disorders. It has built a rich pipeline based on proprietary discovery platforms, TALENTTM, FD2TM and PD2TM.
The company is looking for partners to develop and commercialize the asset globally or regionally.
Asset: Asset 1–CXCR4 antagonist; Asset 2–FGFR and VEGFR dual inhibitor; Asset 2–ALK inhibitor; Asset 4–CDK Inhibitor
Status: Ongoing ph1 (Asset 1, 2 & 3); IND-Enabling (Asset 4)
Indications: Solid tumors and hematopoietic malignancies
Asset 1 Highlights:
- The first oral CXCR4 antagonist medication. No oral CXCR4 antagonist is commercially available yet.
- Clean GPCR selectivity profile. 1μM Asset1 results in 113% inhibition of CXCR4 without any significant effect (EC50/IC50>10μM) on 47 safety-relevant targets.
- Potent hematopoietic stem cell mobilizing effect is observed in animal models. In beagle dogs, the amount of CD34+ cells and whole blood WBC are in a dose-dependent manner and increased significantly at all the low, medium and high concentration groups.l Synergistic with multiple drugs. The combined administration of Asset 1 and G-CSF has a better effect on mouse hematopoietic stem cell mobilization than G-CSF alone.
Asset 2 Highlights:
- Selectively against most other kinases. The target kinase inhibitory activity against FGFR and VEGFR is 2-8 times higher than ODM203.
- Better oral bioavailability (59% in mice, 34% in rats, 57% in dogs) than ODM203 (45% in mice, 10% in rats, 51% in dogs)
- The synergistic effect of inhibiting both FGFR and VEGFR has been confirmed in animal model studies.
- The product shows excellent PK, especially the AUC is 3-fold higher than ODM203. It is predicted that the product just needs half a dose of the ODM203 to achieve the same therapeutic effect in human.
Asset 3 Highlights:
- 2-10 times inhibitory activity than alectinib against ALK.
- Significantly inhibit tumor growth in female Nude Mice bearing NCI-H3122 NSCLC Xenograft. The relative tumor growth rates (T/C) of Asset3 is 2.75% (P < 0.001), versus 47.80% of alectinib compare to vehicle.
- Potent activity against RET kinase and RET-driven tumor cell lines, and IC50 is 150 times lower than that of alectinib.
Asset 4 Highlights:
- Superior efficacy than Abemaciclib and Palbociclib at the same dosage level in AML and MCL mouse orthotopic models. The proportion of hCD4+ cells in bone marrow and blood was significantly reduced as well as the body weight coefficient of spleen in a dose-dependent manner.
- nM-level cytostatic activity in hematological cell lines.
- The product will focus on mutations in acute myeloid leukemia, and there is no CDK inhibitor approved for commercialization for hematological disorders yet.
Download Asset Summary (PDF file) here. If you are interested in any asset, please reply to wxiang@yafocapital.com.
BioToChina.org 